FORMULATION AND EVALUATION OF CLARITHROMYCIN – LOADED SELF – MICRO EMULSIFIED DRUG DELIVERY SYSTEM

Clarithromycin is a lipophilic and poorly water-soluble macrolide antibiotic which belongs to class II of the biopharmaceutics classification system. Its oral absorption and related bioavailability are dissolution rate-limited and relatively low. Subsequently, the formulation of oral clarithromycin delivery systems poses a huge challenge to the formulation scientist. Utilization of self – micro emulsifying drug delivery system technology, with the intent of enhancing oral bioavailability of clarithromycin was designed as this study’s principal objective. Following successful screening studies involving solubility, compatibility and phase evaluations, series of clarithromycin – loaded self – micro emulsifying drug delivery system formulations were developed. Formulations were subjected to optimization and characterization analyses, from which formulation C2A with compositions (% w/w) of olive oil 5%, Tween 80: ethanol (4:1) 94.42%, clarithromycin 0.5% and aspartame 0.08% was optimized. The optimized/ test formulation was subjected to stability, in-vitro drug release, and pharmacokinetic analyses. Estimated parameters included a droplet size of 16.30 ± 3.31 nm, polydispersity index of 0.203 ± 0.11, and zeta potential of -2.01 ± 1.56 millivolts. Test and reference clarithromycin formulations exhibited comparable drug release profiles, inferring pharmaceutical equivalence. The test formulation was stable over a six – month period. No significant difference, at a probability level of 0.05, was observed between the two formulations with respect to pharmacokinetic parameters investigated. Forest plot constructed for test and reference formulations showed compliance with FDA standards, indicating bioequivalence character. The study indicates test formulation’s potential of being used as a possible alternative to reference clarithromycin.